The paradigm of using nanoparticulate pharmaceutical carriers has been well established over the past decade, both in pharmaceutical research and in the clinical setting. Drug carriers are expected to stay in the blood for long time, accumulate in pathological sites with affected and leaky vasculature (tumors, inflammations, and infarcted areas) via the enhanced permeability and retention (EPR) effect, and facilitate targeted delivery of specific ligand-modified drugs and drug carriers into poorly accessible areas. Among various approaches to specifically target drug-loaded carrier systems to required pathological sites in the body, two seem to be most advanced--passive (EPR effect-mediated) targeting, based on the longevity of the pharmaceutical carrier in the blood and its accumulation in pathological sites with compromised vasculature, and active targeting, based on the attachment of specific ligands to the surface of pharmaceutical carriers to recognize and bind pathological cells. Here, we will consider and discuss these two targeting approaches using tumor targeting as an example.